212188-60-8
212188-60-8 结构式
基本信息
BAY 38-7271
BAY-38-7071
O-1861 (R-form)
(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate
(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate USP/EP/BP
4,4,4-Trifluoro-1-butanesulfonic acid 3-[[(2R)-2,3-dihydro-2-(hydroxymethyl)-1H-inden-4-yl]oxy]phenyl ester
1-Butanesulfonic acid, 4,4,4-trifluoro-,3-[[(2R)-2,3-dihydro-2-(hydroxyMethyl)-1H-inden-4-yl]oxy]phenyl ester
物理化学性质
常见问题列表
|
CB1 1.85 nM (Ki) |
CB2 5.96 nM (Ki) |
BAY 38-7271 shows only minor interactions at the micromolar range with other binding sites such as adenosine A
3
receptor (IC
50
= 7.5 μM), peripheral GABA
A
benzodiazepine receptor (IC
50
= 971 nM), melatonin ML
1
receptor (IC
50
= 3.3 μM), and at the monoamine transporter (IC
50
= 1.7 μM).
BAY 38-7271 (Ed
50
= 0.02 mg/kg; i.v. and 0.5 mg/kg; i.p.) induces a potent and dose-de-pendent reduction in core body temperature.
BAY 38-7271 has low physical dependence liability and is not essentially different from that of other cannabinoid CB
1
receptor agonists.
BAY 38-7271 (1-1000 ng/kg/h; i.v. infusion; for 4 hours) shows neuroprotective efficacy in the rat SDH model.
BAY 38-7271 also has neuroprotective efficacy in models of transient and permanent occlusion of the middle cerebral artery and brain edema models.
| Animal Model: | Wistar rat ,TBI rat models (acute subdural hematoma, SDH) |
| Dosage: | 1 ng/kg/h, 10 ng/kg/h, 100 ng/kg/h, 1000 ng/kg/h |
| Administration: | Intravenous infusion, for 4 hours |
| Result: | Reduced the mean infarct volume. |